New SARM GW-501516 - AnabolicMinds.com

New SARM GW-501516

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    New SARM GW-501516


    anyone heard of this? I came across it on a Reaserch Chem site (which is extremely reputable) and this is a SARM i have never come across before- sounds somewhat similar to ostarine

    here is the write up


    FOR RESEARCH PURPOSES ONLY NOT FOR HUMAN CONSUMPTION

    GW-501516
    (also known as GW-501,516,GW1516 or GSK-516) is a PPAR***948; modulator compound being investigated for drug use by GlaxoSmithKline.[1][2] It activates the same pathways activated through exercise, including PPAR***948; and AMP-activated protein kinase. It is being investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. [3] [4] GW-501516 has a synergistic effect when combined with AICAR: the combination has been shown to significantly increase exercise endurance in animal studies more than either compound alone. [5][6]

    GW-50156 regulates fat burning through a number of widespread mechanisms [7]; it increases glucose uptake in skeletal muscle tissue and increases muscle gene expression, especially genes involved in preferential lipid utilization.,[8][9] [10] This shift changes the body's metabolism to favor burning fat for energy instead of carbohydrates or muscle protein, potentially allowing clinical application for obese patients to lose fat effectively without experiencing muscle catabolism or the effects and satiety issues associated with low blood sugar. [11] GW-501516 also increases muscle mass, which improved glucose tolerance and reduced fat mass accumulation even in mice fed a very high fat diet, suggesting that GW-501516 may have a protective effect against obesity [12]

    It has been demonstrated at oral doses of 5 mg a day to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome, most likely by stimulating fatty acid oxidation.[13] Treatments with GW-501516 have been shown to increase HDL cholesterol by up to 79% in rhesus monkeys and the compound is now undergoing Phase II trials to improve HDL cholesterol in humans. [14]

    Concerns were raised prior to the 2008 Beijing Olympics that GW-501516 could be used by athletes as a performance enhancing drug which was not currently controlled by regulations or detected by standard tests. One of the main researchers from the study on enhanced endurance consequently developed a urine test to detect the drug, and made it available to the International Olympic Committee.[15] The World Anti-Doping Agency has also begun work on a test GW-501516 and other related PPAR***948; modulators.,[16] and they have been added to the prohibited list from 2009 onwards.[17] The compound has yet to be named a controlled or prohibited substance by any nation's drug enforcement or regulation agency. To date, no athlete is known to have tested positive for the substance, though the increase in endurance, muscle fiber performance, fat loss and metabolism suggests GW-501516 has the potential for ergogenic use and abuse.
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    Subbed for more info.
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    interesting
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    Pat talked about this over at his forum. Said the stuff is great for endurance but horrible for strength.
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    It has been getting great reviews at least one other board. Results starting almost immediately. No sides noticed by reviewers though I haven't seen anyone post bloodwork.
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    This is not a SARM. It is a PPAR delta agonist not an androgen. Pat is right. good for endurance, will probably lower cholesterol but no evidence that I know of for anabolic action.
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    Quote Originally Posted by pumpga
    It has been getting great reviews at least one other board. Results starting almost immediately. No sides noticed by reviewers though I haven't seen anyone post bloodwork.
    Hmmm. Anyone report on suppression/dosing?
    I can it being used on a hardening routine with very good results.
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    Quote Originally Posted by sethroberts View Post
    This is not a SARM. It is a PPAR delta agonist not an androgen. Pat is right. good for endurance, will probably lower cholesterol but no evidence that I know of for anabolic action.
    funny the site is selling it under SARMs catagory. I have always had good interactions with these guys so maybe they are mistaken. it says that it regulates glucose uptake, and helps with fat oxidation- i am insulin resistant- so this would help me lean out perhaps?
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    Like most people in this industry (supps, research chems) they either don't know what they are talking about or are deliberately lieing to sell more product. It doesn't take a science degree to buy raw materials from china, package them and sell them.
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    Any studies or blood work on how suppressive PPARs are?
    And uses?
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    seth can you chime in about how this PPAR might help me reduce bodyfat via increased glucose uptake and fat oxidation? I am insulin resitant- just how effective would this product be?
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    Quote Originally Posted by mattrag View Post
    Hmmm. Anyone report on suppression/dosing?
    I can it being used on a hardening routine with very good results.
    Dosing was 10mg, nothing about suppression. It was an Ostarine and GW501516 cycle. Reviewer was seeing some gains while leaning out with increase in endurance.
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    I honestly don't know. It was originally researched to reduce cholesterol and reduce body weight. It was effective in these regards but I know there were concerns at the time (2002 or so) that it might promote tumor growth.
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    It's the no-work fat loss from the PPAR-beta agonism that makes it appealing for bbers


    Quote Originally Posted by sethroberts View Post
    This is not a SARM. It is a PPAR delta agonist not an androgen. Pat is right. good for endurance, will probably lower cholesterol but no evidence that I know of for anabolic action.
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    The guy I saw was using 5 mg and lost a decent amount of fat. He was not fat to begin with. He ramped up to 7.5 mg and it became very uncomfortable with respect to sweating/body heat.

    Quote Originally Posted by pumpga View Post
    Dosing was 10mg, nothing about suppression. It was an Ostarine and GW501516 cycle. Reviewer was seeing some gains while leaning out with increase in endurance.
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    Cool


    Quote Originally Posted by Whacked View Post
    It's the no-work fat loss from the PPAR-beta agonism that makes it appealing for bbers
    Thanks for the education
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    Quote Originally Posted by Whacked
    The guy I saw was using 5 mg and lost a decent amount of fat. He was not fat to begin with. He ramped up to 7.5 mg and it became very uncomfortable with respect to sweating/body heat.
    Wow. Super interesting. Did he mention what other sides and sups he was on?
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    Seth: I smell sacrcasm. LOL

    This drug is is gaining a rep as an endurance enthusiast's dream drug (as you also pointed out). I was merely letting the viewers know WHY this drug has is appealing for aesthetic reasons as well based on your earlier response:

    Quote Originally Posted by sethroberts View Post
    I honestly don't know. It was originally researched to reduce cholesterol and reduce body weight. It was effective in these regards but I know there were concerns at the time (2002 or so) that it might promote tumor growth.
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    No sides until he ramped it up to 7.5 mg (from 5mg/day)

    At the increased dosing schedule, increased sweat was alll that I recall him noting

    That said, I wouldnt trust this stuff just yet

    Let the dust settle and be sure to get in a copious dose of PPAR-alpha supps (fish and sesamin) which impart some fat loss in addition to havign other health benefits.

    Quote Originally Posted by mattrag View Post
    Wow. Super interesting. Did he mention what other sides and sups he was on?
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    Unless I was getting frequent bloods and other health parameter checks I wouldn't take this just yet. I'd rather know what sides to look for than learn of the sides.
    Thanks for your insight!
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    Good discussion here. More things coming out every day it seems (how legit or useful or safe they are is obviously suspect).
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    I concur

    Quote Originally Posted by mattrag View Post
    Unless I was getting frequent bloods and other health parameter checks I wouldn't take this just yet. I'd rather know what sides to look for than learn of the sides.
    Thanks for your insight!
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    so what exactly does this do? Matty, would this be suitable for me bro? you know what my goals
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    Quote Originally Posted by runner_79 View Post
    so what exactly does this do? Matty, would this be suitable for me bro? you know what my goals
    Hmm, I really dont know. If this thing could do what it did w/o any adverse effects it'd be basically cardio in a bottle it seems. PPAR b-agonist. Kinda scared though... not enough research or people using it to tell for sure if it is "safe" to use.
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    Yeah. My Aussie supplier has a few bottles.
    Also has mdrol clone...hmmmm interested in mdrol clone called super mass

    What about d-zine(co. That makes forged burner)
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    I'd like to hear more on this. In for more discussion
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    Activation of nuclear hormone receptor peroxisome proliferator***8211;activated receptor-***948; accelerates intestinal adenoma growth

    Rajnish A Gupta1, Dingzhi Wang1, Sharada Katkuri1, Haibin Wang2, Sudhansu K Dey2 & Raymond N DuBois1,2,3

    Abstract

    We treated Apcmin mice, which are predisposed to intestinal polyposis, with a selective synthetic agonist of peroxisome proliferator***8211;activated receptor-***948; (PPAR-***948. Exposure of Apcmin mice to the PPAR-***948; ligand GW501516 resulted in a significant increase in the number and size of intestinal polyps. The most prominent effect was on polyp size; mice treated with the PPAR-***948; activator had a fivefold increase in the number of polyps larger than 2 mm. Our results implicate PPAR-***948; in the regulation of intestinal adenoma growth.

    This link has more information: carcin.oxfordjournals.org/content/28/12/2641.full
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    Intestinal polyps aren't anything I want LOL
    Quote Originally Posted by alwaysgaining View Post
    I've also done fasting and doseing and felt grealt anabolicness , deffint hunger but I'm stronger than that keep full and vascular and strength gose up
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    Quote Originally Posted by swollen87
    Intestinal polyps aren't anything I want LOL
    Yea for sure.
    Looks like this compound I will avoid.
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    i might have rushed this purchase a bit. i got an email saying half off at a certain site, so i checked it out expecting to get a bottle of s-4 for cheap, but then i saw this and read up a bit on it. ended buying a bottle of it but now im thinking i shouldnt have. intestinal polyps sound very un-fun. then again, that was with rats that were predisposed to intestinal polyps.
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    Quote Originally Posted by pumpga View Post
    Dosing was 10mg, nothing about suppression. It was an Ostarine and GW501516 cycle. Reviewer was seeing some gains while leaning out with increase in endurance.
    Oral or sub Q? Or other? Thanks.
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    Bro

    NEVER inject ANY research product man. All of it is intended for ORAL consumption

    The ONLY exceptions are products that require reconstitution (bacteriostatic water or acetic acid needs to be ADDED to the powder). Examples of these include: Peptides (tanning peptides-melanotoan, GH-peptides/analogues, IGF, etc) and HCG

    Quote Originally Posted by motiv8er View Post
    Oral or sub Q? Or other? Thanks.
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    Interesting compound. It will be interesting to see how many more studies are published on this over the next year or so. The essential reversal of insulin resistance would be very promising. While the intestinal polyps would obviously be a major con, as was pointed out, it was in mice predisposed to them. That being said, I'd still wait to see more research before messing with a compound like this.
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    Quote Originally Posted by Whacked View Post
    Bro

    NEVER inject ANY research product man. All of it is intended for ORAL consumption

    The ONLY exceptions are products that require reconstitution (bacteriostatic water or acetic acid needs to be ADDED to the powder). Examples of these include: Peptides (tanning peptides-melanotoan, GH-peptides/analogues, IGF, etc) and HCG
    Cool. I was looking at many new peptides and didnt know how this one functioned. Thanks.
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    there is a thread a right above this one with a guy that is running it right now.....
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    In case you didnt see:

    Study on Obese Humans
    OBJECTIVE— Pharmacological use of peroxisome proliferator–activated receptor (PPAR)δ agonists and transgenic overexpression of PPARδ in mice suggest amelioration of features of the metabolic syndrome through enhanced fat oxidation in skeletal muscle. We hypothesize a similar mechanism operates in humans.

    RESEARCH DESIGN AND METHODS— The PPARδ agonist (10 mg o.d. GW501516), a comparator PPARα agonist (20 μg o.d. GW590735), and placebo were given in a double-blind, randomized, three-parallel group, 2-week study to six healthy moderately overweight subjects in each group. Metabolic evaluation was made before and after treatment including liver fat quantification, fasting blood samples, a 6-h meal tolerance test with stable isotope fatty acids, skeletal muscle biopsy for gene expression, and urinary isoprostanes for global oxidative stress.

    RESULTS— Treatment with GW501516 showed statistically significant reductions in fasting plasma triglycerides (−30%), apolipoprotein B (−26%), LDL cholesterol (−23%), and insulin (−11%), whereas HDL cholesterol was unchanged. A 20% reduction in liver fat content (P < 0.05) and 30% reduction in urinary isoprostanes (P = 0.01) were also observed. Except for a lowering of triglycerides (−30%, P < 0.05), none of these changes were observed in response to GW590735. The relative proportion of exhaled CO2 directly originating from the fat content of the meal was increased (P < 0.05) in response to GW501516, and skeletal muscle expression of carnitine palmitoyl-transferase 1b (CPT1b) was also significantly increased.

    CONCLUSIONS— The PPARδ agonist GW501516 reverses multiple abnormalities associated with the metabolic syndrome without increasing oxidative stress. The effect is probably caused by increased fat oxidation in skeletal muscle.

    Study on Lean Individuals
    Objectives— Exercise increases fatty acid oxidation (FAO), improves serum high density lipoprotein cholesterol (HDLc) and triglycerides (TG), and upregulates skeletal muscle peroxisome proliferator activated receptor (PPAR)δ expression. In parallel, PPARδ agonist-upregulated FAO would induce fatty-acid uptake (via peripheral lipolysis), and influence HDLc and TG-rich lipoprotein particle metabolism, as suggested in preclinical models.

    Methods and Results— Healthy volunteers were allocated placebo (n=6) or PPARδ agonist (GW501516) at 2.5 mg (n=9) or 10 mg (n=9), orally, once-daily for 2 weeks while hospitalized and sedentary. Standard lipid/lipoproteins were measured and in vivo fat feeding studies were conducted. Human skeletal muscle cells were treated with GW501516 in vitro and evaluated for lipid-related gene expression and FAO. Serum TG trended downwards (P=0.08, 10 mg), whereas TG clearance post fat-feeding improved with drug (P=0.02). HDLc was enhanced in both treatment groups (2.5 mg P=0.004, 10 mg P<0.001) when compared with the decrease in the placebo group (−11.51.6%, P=0.002). These findings complimented in vitro cell culture results whereby GW501516 induced FAO and upregulated CPT1 and CD36 expression, in addition to a 2-fold increase in ABCA1 (P=0.002). However, LpL expression remained unchanged.

    Conclusions— This is the first report of a PPARδ agonist administered to man. In this small study, GW501516 significantly influenced HDLc and TGs in healthy volunteers. Enhanced in vivo serum fat clearance, and the first demonstrated in vitro upregulation in human skeletal muscle fat utilization and ABCA1 expression, suggests peripheral fat utilization and lipidation as potential mechanisms toward these HDL:TG effects.
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    Definitely looks like something to avoid.
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    why? because it caused intestinal polyps in animals that were already predisposed to them?
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    Quote Originally Posted by ManBeast View Post
    why? because it caused intestinal polyps in animals that were already predisposed to them?
    Have you shelled out $1000 dollars to have your genome analyzed to see what kind of conditions you're predisposed to? I haven't. Not to mention not only do we not know what half of the genome is responsible for, we still have very little grasp over the enormous net of interactions between proteins, transcription factors, and all other transcriptional/translational/post-translational regulators in our bodies. Taking something like this knowing that it has been implicated in the growth of benign tumors is reckless without having more studies. You can do what you want with your body, but I know at my young age I'm not taking something like this knowing the potential risks only to face those consequences down the line.
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    Quote Originally Posted by Torobestia View Post
    Have you shelled out $1000 dollars to have your genome analyzed to see what kind of conditions you're predisposed to? I haven't. Not to mention not only do we not know what half of the genome is responsible for, we still have very little grasp over the enormous net of interactions between proteins, transcription factors, and all other transcriptional/translational/post-translational regulators in our bodies. Taking something like this knowing that it has been implicated in the growth of benign tumors is reckless without having more studies. You can do what you want with your body, but I know at my young age I'm not taking something like this knowing the potential risks only to face those consequences down the line.
    With regards to health, I think this is a very conservative approach (avoiding this). BUT, if you dont take it you'll never know. And some people are willing to take that risk. I wouldn't really discourage intaking unknown chemicals that show some form of bad side effect but ONLY if you know the side effects and are willing to accept them. I take PH/DS and I know i could be saying good bye to my fatherhood, I know I might never come back, BUT I will take ALL precautions via AI, SERMs, Test boosters, minerals, etc. To assure I am safest I can be. If I castrate myself by doing so its my fault. I will report it but I will not blame anyone but myself. I will not say don't take XXXXX supp because it messes you up! Or Im gonna sue XXXX supp company because they sell it! I took it, I knew it was risky. I HAVE GW. I won't take it until I see more studies/logs. Only reason I have it though is because I am stocking up on ALL supps as I am paranoid and I think the FDA is gonna ban EVERYTHING, thus raising the price on all the stuff out there now.
    RecoverBro ELITE
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